摘要
艾沙康唑是一种三唑类广谱抗真菌药,该药以水溶性前药硫酸艾沙康唑鎓的形式静脉注射或口服给药,它能通过抑制真菌细胞色素P45014DM的生物功能干扰其细胞壁的形成,最终达到抗真菌的作用。本文综述艾沙康唑、水溶性侧链结构片段及硫酸艾沙康唑鎓的合成方法,并对合成路线的优缺点进行评述,为硫酸艾沙康唑鎓工艺的开发奠定基础。
Isavuconazole is a broad-spectrum triazole antifungal agent,which is administered as a water-soluble prodrug-isavuconazonium sulfate. Recently,its oral and intravenous formulations are available. Isavuconazole inhibits fungal cytochrome P45014 DM,thus interferes with the biological function of cell wall formation and plays the antifungal role. In this paper,we summarize the synthetic methods of isavuconazole,water-soluble segments of side chain and isavuconazonium sulfate and evaluate their advantages and disadvantages,which lays a foundation for isavuconazonium sulfate technology development.
出处
《国际药学研究杂志》
CAS
CSCD
北大核心
2016年第3期436-440,444,共6页
Journal of International Pharmaceutical Research
关键词
抗真菌药
艾沙康唑
水溶性侧链结构片段
合成
药物化学
antifungal agent
isavuconazole
water-soluble segments of side chain
isavuconazonium sulfate
synthesis
pharmaceutical chemistry
